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- W2166501811 startingPage "43" @default.
- W2166501811 abstract "The endogenous cannabinoid (CB) (endocannabinoid) signaling system is involved in a variety of (patho)physiological processes, primarily by virtue of natural, arachidonic acid-derived lipids (endocannabinoids) that activate G protein-coupled CB1 and CB2 receptors. A hyperactive endocannabinoid system appears to contribute to the etiology of several disease states that constitute significant global threats to human health. Consequently, mounting interest surrounds the design and profiling of receptor-targeted CB antagonists as pharmacotherapeutics that attenuate endocannabinoid transmission for salutary gain. Experimental and clinical evidence supports the therapeutic potential of CB1 receptor antagonists to treat overweight/obesity, obesity-related cardiometabolic disorders, and substance abuse. Laboratory data suggest that CB2 receptor antagonists might be effective immunomodulatory and, perhaps, anti-inflammatory drugs. One CB1 receptor antagonist/inverse agonist, rimon-abant, has emerged as the first-in-class drug approved outside the United States for weight control. Select follow-on agents (taranabant, otenabant, surinabant, rosonabant, SLV-319, AVE1625, V24343) have also been studied in the clinic. However, rimonabant's market withdrawal in the European Union and suspension of rimonabant's, taranabant's, and otenabant's ongoing development programs have highlighted some adverse clinical side effects (especially nausea and psychiatric disturbances) of CB1 receptor antagonists/inverse agonists. Novel CB1 receptor ligands that are peripherally directed and/or exhibit neutral antagonism (the latter not affecting constitutive CB1 receptor signaling) may optimize the benefits of CB1 receptor antagonists while minimizing any risk. Indeed, CB1 receptor-neutral antagonists appear from preclinical data to offer efficacy comparable to or better than that of prototype CB1 receptor antagonists/inverse agonists, with less propensity to induce nausea. Continued pharmacological profiling, as the prelude to first-in-man testing of CB1 receptor antagonists with unique modes of targeting/pharmacological action, represents an exciting translational frontier in the critical path to CB receptor blockers as medicines." @default.
- W2166501811 created "2016-06-24" @default.
- W2166501811 creator A5000540926 @default.
- W2166501811 creator A5045369109 @default.
- W2166501811 date "2009-02-27" @default.
- W2166501811 modified "2023-10-18" @default.
- W2166501811 title "Cannabinoid receptor antagonists: pharmacological opportunities, clinical experience, and translational prognosis" @default.
- W2166501811 cites W1491109154 @default.
- W2166501811 cites W1495173924 @default.
- W2166501811 cites W1669871566 @default.
- W2166501811 cites W1824285398 @default.
- W2166501811 cites W1875725323 @default.
- W2166501811 cites W1876729781 @default.
- W2166501811 cites W192756024 @default.
- W2166501811 cites W1953204375 @default.
- W2166501811 cites W1964037009 @default.
- W2166501811 cites W1967012457 @default.
- W2166501811 cites W1967951613 @default.
- W2166501811 cites W1968741339 @default.
- W2166501811 cites W1971036356 @default.
- W2166501811 cites W1971154201 @default.
- W2166501811 cites W1971698096 @default.
- W2166501811 cites W1975454274 @default.
- W2166501811 cites W1975748753 @default.
- W2166501811 cites W1976813870 @default.
- W2166501811 cites W1977256878 @default.
- W2166501811 cites W1979165845 @default.
- W2166501811 cites W1979456416 @default.
- W2166501811 cites W1980950685 @default.
- W2166501811 cites W1980988460 @default.
- W2166501811 cites W1982538469 @default.
- W2166501811 cites W1985158305 @default.
- W2166501811 cites W1985712631 @default.
- W2166501811 cites W1987669663 @default.
- W2166501811 cites W1991224894 @default.
- W2166501811 cites W1991778481 @default.
- W2166501811 cites W1991898746 @default.
- W2166501811 cites W1993764059 @default.
- W2166501811 cites W1994145229 @default.
- W2166501811 cites W1995338592 @default.
- W2166501811 cites W1995552285 @default.
- W2166501811 cites W1997488482 @default.
- W2166501811 cites W1998862968 @default.
- W2166501811 cites W2002879860 @default.
- W2166501811 cites W2007323738 @default.
- W2166501811 cites W2009495434 @default.
- W2166501811 cites W2011302013 @default.
- W2166501811 cites W2011754496 @default.
- W2166501811 cites W2014177873 @default.
- W2166501811 cites W2015264989 @default.
- W2166501811 cites W2015829020 @default.
- W2166501811 cites W2016079672 @default.
- W2166501811 cites W2018115671 @default.
- W2166501811 cites W2021047896 @default.
- W2166501811 cites W2021211846 @default.
- W2166501811 cites W2024331925 @default.
- W2166501811 cites W2024951820 @default.
- W2166501811 cites W2025025939 @default.
- W2166501811 cites W2026010581 @default.
- W2166501811 cites W2026530510 @default.
- W2166501811 cites W2027604293 @default.
- W2166501811 cites W2028981383 @default.
- W2166501811 cites W2029918787 @default.
- W2166501811 cites W2030159344 @default.
- W2166501811 cites W2031325755 @default.
- W2166501811 cites W2033981979 @default.
- W2166501811 cites W2039964546 @default.
- W2166501811 cites W2045245889 @default.
- W2166501811 cites W2045544544 @default.
- W2166501811 cites W2047029495 @default.
- W2166501811 cites W2050022483 @default.
- W2166501811 cites W2051423896 @default.
- W2166501811 cites W2051554315 @default.
- W2166501811 cites W2052172874 @default.
- W2166501811 cites W2053586784 @default.
- W2166501811 cites W2054485560 @default.
- W2166501811 cites W2055000265 @default.
- W2166501811 cites W2056505887 @default.
- W2166501811 cites W2057333363 @default.
- W2166501811 cites W2059479437 @default.
- W2166501811 cites W2062962038 @default.
- W2166501811 cites W2063663168 @default.
- W2166501811 cites W2070178149 @default.
- W2166501811 cites W2071649073 @default.
- W2166501811 cites W2075647580 @default.
- W2166501811 cites W2079105522 @default.
- W2166501811 cites W2085314208 @default.
- W2166501811 cites W2085520160 @default.
- W2166501811 cites W2085570274 @default.
- W2166501811 cites W2087587748 @default.
- W2166501811 cites W2087592645 @default.
- W2166501811 cites W2089543709 @default.
- W2166501811 cites W2090772580 @default.
- W2166501811 cites W2092509345 @default.
- W2166501811 cites W2092554151 @default.
- W2166501811 cites W2095139799 @default.
- W2166501811 cites W2095489324 @default.
- W2166501811 cites W2095688984 @default.